Pharmacokinetics Flashcards

1
Q

Recall the 7 major routes by which drugs can be administered

A
  1. IV
  2. Intraperitoneal
  3. Oral
  4. Intramuscular
  5. Dermal
  6. Subcutaneous
  7. Inhalation
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2
Q

Recall an advantage and disadvantage of intraperitoneal administration

A

Advantage: richly perfused area
Disadvantage: requires training

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3
Q

Recall an advantage and disadvantage of drug inhalation

A

Advantage: well perfused region
Disadvantage: Danger with powder

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4
Q

Recall an advantage of dermal administration of a drug

A

Slow, sustained release

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5
Q

Recall an advantage and disadvantage of IV administration of a drug

A

Advantage: very rapid onset
Disadvantage: requires training

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6
Q

Recall 4 methods by which a drug might pass through a lipid bilayer

A
  1. Diffusion (if non-polar)
  2. Diffuse across aqueous pore (if polar)
  3. Carrier molecule
  4. Pinocytosis
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7
Q

Why do drugs often exist in both ionised and non-ionised forms?

A

Non-ionised form will easily cross lipid bilayer, ionised form will travel around body more easily

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8
Q

What affects the ratio of ionised: non-ionised drug?

A

pH

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9
Q

What is the pKa of aspirin?

A

3.4

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10
Q

Where does the majority of aspirin absorption take place and why?

A

Stomach - more of the unionised form here (driven by low pH) and so diffuses across lipid bilayer more easily

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11
Q

What is “ion trapping”?

A

Drug gets stuck in ionised form in aqueous compartment (?)

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12
Q

Recall the 4 factors affecting drug distribution

A
  1. Regional blood flow
  2. Extracellular binding to plasma proteins
  3. Capillary permeability
  4. Tissue localisation
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13
Q

How does protein-binding affect drug distribution?

A

Protein-bound drug no longer available for absorption

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14
Q

What sort of drugs are most likely to sjow tissue localisation?

A

Lipophillic drugs - accumulate in fatty tissue such as testes and brain

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15
Q

What are the 2 major routes of excretion of drugs?

A

Liver and Kidney

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16
Q

What sort of drugs tend to be excreted via the liver?

A

Drugs with a high MR that are lipophilic (dissolved in bile)

17
Q

How may lipophobic drugs enter the bile

A

Active transport mechanisms - eg glucuronides

18
Q

What problem may be caused by biliary excretion?

A

Enterohepatic cycling

19
Q

How do drugs enter the urine once they have reached the kidney?

A

Active secretion (NOT ultrafiltration as large protein-bound complexes cannot be filtered)

20
Q

What compound is used to increase aspirin secretion?

A

IV NaHCO3

21
Q

Explain why IV sodium bicarbonate increases aspirin secretion

A
  1. NaHCO3 increases urine pH
  2. Aspirin is ionised –> less lipid soluble
  3. Less aspirin reabsorbed
22
Q

What is “first pass metabolism”?

A

The concentration of a drug is greatly reduced before it reaches the systemic circulation, first passing through the hepatic circulation.

23
Q

Define “enterohepatic circulation”

A

Drug/ metabolite excreted into gut (via bile) then reabsorbed, taken to liver and excreted again

24
Q

What is first-order kinetics?

A

When the half life of a drug is constant

25
Q

What is zero-order kinetics?

A

Drug is being eliminated at a constant rate

26
Q

Define “bioavailability”

A

Proportion of administered drug available within body to exert pharmacological effect

27
Q

Upon which 2 factors does drug clearance depend?

A
  1. Volume of distribution

2. Rate of drug elimination

28
Q

Recall the equation used to calculate clearance for drugs that are cleared by first order kinetics

A

Volume of distribution = Kel (log2/ half life)

29
Q

Recall the equation used to calculate clearance for drugs that are cleared by zero order kinetics

A

Time x Kel (change in conc/ change in time)

30
Q

What is drug clearance?

A

Sum of metabolism by both liver and kidneys